HRP20191220T1 - Disupstituirani oktahi-dropirolo[3,4-c]piroli kao modulatori oreksin receptora - Google Patents
Disupstituirani oktahi-dropirolo[3,4-c]piroli kao modulatori oreksin receptora Download PDFInfo
- Publication number
- HRP20191220T1 HRP20191220T1 HRP20191220TT HRP20191220T HRP20191220T1 HR P20191220 T1 HRP20191220 T1 HR P20191220T1 HR P20191220T T HRP20191220T T HR P20191220TT HR P20191220 T HRP20191220 T HR P20191220T HR P20191220 T1 HRP20191220 T1 HR P20191220T1
- Authority
- HR
- Croatia
- Prior art keywords
- phenyl
- triazol
- chemical entity
- pharmaceutically acceptable
- pyrimidin
- Prior art date
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- 108050000742 Orexin Receptor Proteins 0.000 title claims 2
- 102000008834 Orexin receptor Human genes 0.000 title claims 2
- 150000003233 pyrroles Chemical class 0.000 title 1
- -1 CO2C1-4alkyl Chemical group 0.000 claims 77
- 150000005829 chemical entities Chemical class 0.000 claims 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 14
- 239000000546 pharmaceutical excipient Substances 0.000 claims 12
- 125000005843 halogen group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 208000019116 sleep disease Diseases 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 3
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000000389 2-pyrrolyl group Chemical group [H]N1C([*])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims 3
- CKJNUZNMWOVDFN-UHFFFAOYSA-N methanone Chemical compound O=[CH-] CKJNUZNMWOVDFN-UHFFFAOYSA-N 0.000 claims 3
- 125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 208000020685 sleep-wake disease Diseases 0.000 claims 3
- 150000003852 triazoles Chemical group 0.000 claims 3
- WCYWZMWISLQXQU-FIBGUPNXSA-N trideuteriomethane Chemical compound [2H][C]([2H])[2H] WCYWZMWISLQXQU-FIBGUPNXSA-N 0.000 claims 3
- OQHVVOYDDRBQRI-UHFFFAOYSA-N 4-(trifluoromethyl)pyrimidine-5-carboxylic acid Chemical group OC(=O)C1=CN=CN=C1C(F)(F)F OQHVVOYDDRBQRI-UHFFFAOYSA-N 0.000 claims 2
- LHRIUKSRPHFASO-UHFFFAOYSA-N 6-methyl-1h-pyrimidin-4-one Chemical group CC1=CC(=O)N=CN1 LHRIUKSRPHFASO-UHFFFAOYSA-N 0.000 claims 2
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims 2
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 2
- ULXUMMWTPGKPRC-UHFFFAOYSA-N [2-(4,6-dimethylpyrimidin-2-yl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-[4-methoxy-2-(triazol-2-yl)phenyl]methanone Chemical group N1=CC=NN1C1=CC(OC)=CC=C1C(=O)N(CC1C2)CC1CN2C1=NC(C)=CC(C)=N1 ULXUMMWTPGKPRC-UHFFFAOYSA-N 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 206010022437 insomnia Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- YEBKRKAIWOXVDB-UHFFFAOYSA-N n,n,6-trimethylpyrimidin-4-amine Chemical group CN(C)C1=CC(C)=NC=N1 YEBKRKAIWOXVDB-UHFFFAOYSA-N 0.000 claims 2
- NQTRKOJHWJWPQL-UHFFFAOYSA-N 6-methylpyrimidine-4-carbonitrile Chemical group CC1=CC(C#N)=NC=N1 NQTRKOJHWJWPQL-UHFFFAOYSA-N 0.000 claims 1
- YSRGRWJKRYESQW-UHFFFAOYSA-N 6-methylpyrimidine-4-carboxylic acid Chemical group CC1=CC(C(O)=O)=NC=N1 YSRGRWJKRYESQW-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 102000002512 Orexin Human genes 0.000 claims 1
- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
- 150000003840 hydrochlorides Chemical class 0.000 claims 1
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 claims 1
- NBGDIFCTCIUDNH-UHFFFAOYSA-N n,n,4-trimethylpyrimidine-2-carboxamide Chemical group CN(C)C(=O)C1=NC=CC(C)=N1 NBGDIFCTCIUDNH-UHFFFAOYSA-N 0.000 claims 1
- CXXSUAVALNOLIP-UHFFFAOYSA-N n,n-dimethyl-4-(trifluoromethyl)pyrimidine-5-carboxamide Chemical group CN(C)C(=O)C1=CN=CN=C1C(F)(F)F CXXSUAVALNOLIP-UHFFFAOYSA-N 0.000 claims 1
- 108060005714 orexin Proteins 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003230 pyrimidines Chemical group 0.000 claims 1
- 208000022925 sleep disturbance Diseases 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
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- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Claims (17)
1. Kemijski entitet koji je spoj formule (I):
gdje:
R1 je fenil supstituiran ili nesupstituiran sa jednim ili dva Ra članova i supstituiran u orto položaju sa Rb;
Ra je halo, C1-4alkil, ili C1-4alkoksi;
Rb je triazol ili pirimidin supstituiran ili nesupstituiran sa halo ili C1-4alkil;
R2 je 6-člani heteroarilni prsten koji sadrži dva atoma dušika supstituirana sa jednim ili više članova izabranim iz grupe koju čine: halo, C1-4alkil, CD3, D, C1-4alkoksi, ciklopropil, morfolin-2-il, CO2C1-4alkil, CO2H, CH2OH, C(O)N(C1-4alkil)2, CF3, CN, OH, NO2, N(C1-4alkil)2, fenil, furan-2-il, tiofen2-il, 1H-pirazol-4-il, i pirolidin-1-il;
ili farmaceutski prihvatljiva sol spoja formule (I).
2. Kemijski entitet prema zahtjevu 1, gdje R1 je (1-metiletil)-2-(2H-1,2,3-triazol-2-il)fenil, 2-(1H-1,2,3-triazol-1il)fenil, 2-(2H-1,2,3-triazol-2-il)fenil, 2-fluoro-6-(2H-1,2,3-triazol-2-il)fenil, 2-metil-6-(2H-1,2,3-triazol-2il)fenil, 3-fluoro-2-(2H-1,2,3-triazol-2-il)fenil, 3-fluoro-2-(1H-1,2,3-triazol-1-il)fenil, 3-metoksi-2-(1H-1,2,3triazol-1-il)fenil, 3-metoksi-2-(2H-1,2,3-triazol-2-il)fenil, 3-metil-2-(2H-1,2,3-triazol-2-il)fenil, 3-metil2-(1H-1,2,3-triazol-1-il)fenil, 4-fluoro-2-(2H-1,2,3-triazol-2-il)fenil, 4-metoksi-2-(2H-1,2,3-triazol-2-il)fenil, 4-metoksi-2-(1H-1,2,3-triazol-2-il)fenil, 4,5-dimetoksi-2-[1,2,3]triazol-1-il-fenil, 4,5-dimetoksi-2-[1,2,3]triazol-2-il-fenil, 5-hloro-2-(2H-1,2,3-triazol-2-il)fenil, 5-fluoro-2-(2H-1,2,3-triazol-2-il)fenil, 5-jodo-2-(2H1,2,3-triazol-2-il)fenil, 5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil, 5-metil-2-(2H-1,2,3-triazol-2-il)fenil, 2-(1H-1,2,4-triazol-1-il)fenil, 2-(1H-1,2,4-triazol-5-il)fenil, 2-(1-metil-1H-1,2,4-triazol-5-il)fenil, 2-(1-metil-1H-1,2,4-triazol-3-il)fenil, 2-(4H-1,2,4-triazol-3-il)fenil, 2-(4H-1,2,4-triazol-4-il)fenil, ili 4,5-difluoro2-(4H-1,2,4-triazol-4-il)fenil).
3. Kemijski entitet prema zahtjevu 1 ili 2, gdje R2 je pirimidin supstituiran sa jednim ili više članova nezavisno izabranim iz grupe koju čine -CI, -F, -CH3, -CF3, -N(CH3)2, -D, ili -CD3.
4. Kemijski entitet prema zahtjevu 1 ili 2, gdje R2 je 4,6-dimetilpirimidin-2-il, 4,5-dimetilpirimidin-2-il, 4,6-dimetoksipirimidin-2-il,4-fenil-pirimidin-2-il, 4-furan-2-ilpirimidin-2-il, 4-metilpirimidin-2-il, 4-metoksipirimidin-2il, 4-tiofen-2-ilpirimidin-2-il, N,N,6-trimetil-pirimidin-4-amin, 4-(trifluorometil)pirimidin-2-il, 4,5,6-trimetilpirimidin-2-il, 4-(trifluorometil)pirimidin-5-karboksilat, 4-(trifluorometil)pirimidin-5-karboksilna kiselina, 5-nitropirimidin-2-il, 6-metilpirimidin-4-karboksilna kiselina, N,N-dimetil-4-(trifluorometil)pirimidin-5-karboksamid, N,N,6-trimetilpirimidin-karboksamid, 6-metilpirimidin-4-karbonitril, 4,6-bis(trifluorometil)pirimidin-2-il, 6metil-pirimidin-4-ol, 4-(furan-2-il)-6-metilpirimidin-2-il, 5-fluoro-4-metilpirimidin-2-il, 5-fluoropirimidin-2-il, 4-metoksi-6-metilpirimidin-2-il, 4-etil-6-metilpirimidin-2-il, 4-izopropil-6-metilpirimidin-2-il, 4-tercbutil-6metilpirimidin-2-il, 4-ciklopropil-6-metilpirimidin-2-il, 4-metil-6-morfolin-4-ilpirimidin-2-il, 5-hloro-4metilpirimidin-2-il, 5-hloro-4,6-dimetilpirimidin-2-il, 5-fluoro-4,6-dimetilpirimidin-2-il, 5-trifluorometilpirimidin-2-il, 4,6-bis[(2H3)metil](2H)pirimidin-2-il, ili 5-etil-4,6-dimetilpirimidin-2-il.
5. Kemijski entitet prema zahtjevu 1 ili 2, gdje R2 je 4,6-dimetilpirimidin-2-il, 4,5-dimetilpirimidin-2-il, 4,6-dimetoksipirimidin-2-il, 4-metilpirimidin-2-il, 4-metoksipirimidin-2-il, N,N,6-trimetil-pirimidin-4-amin, 4-(trifluorometil)pirimidin-2-il, 4,5,6-trimetilpirimidin-2-il, 4,6-bis(trifluorometil)pirimidin-2-il, 6-metil-pirimidin-4-ol, 5-fluoro-4-metilpirimidin-2-il, 5-fluoropirimidin-2-il, 4-metoksi-6-metilpirimidin-2-il, 5-hloro-4-metilpirimidin-2-il, 5-hloro-4,6-dimetilpirimidin-2-il, 5-fluoro-4,6-dimetilpirimidin-2-il, 5-trifluorometilpirimidin-2-il, ili 4,6-bis[(2H3)metil](2H)pirimidin-2-il.
6. Farmaceutski sastav za liječenje bolesti, poremećaja ili medicinskih stanja posredovanih aktivnošću oreksina, koji sadrži:
(a) efikasnu količinu barem jednog kemijskog entiteta formule (I):
gdje:
R1 je fenil supstituiran ili nesupstituiran sa jednim ili dva Račlanovai supstituiran u orto položaju sa Rb;
Ra je halo, C1-4alkil, ili C1-4alkoksi;
Rb je triazol ili pirimidin supstituiran ili nesupstituiran sa halo ili C1-4alkil;
R2 je 6-člani heteroarilni prsten koji sadrži dva atoma dušika kao člana supstituirana sa jednim ili više članova izabranim iz grupe koju čine: halo, C1-4alkil, CD3, D, C1-4alkoksi, ciklopropil, morfolin-2-il, CO2C1-4alkil, CO2H, CH2OH, C(O)N(C1-4alkil)2, CF3, CN, OH, NO2, N(C1-4alkil)2, fenil, furan-2-il, tiofen-2-il, 1H-pirazol-4-il, i pirolidin-1-il;
ili farmaceutski prihvatljiva sol spoja formule (I); i
(b) barem jednu farmaceutski prihvatljivu pomoćnu tvar.
7. Barem jedan kemijski entitet spoja formule (I):
gdje:
R1 je fenil supstituiran ili nesupstituiran sa jednim ili dva Ra članova i supstituiran u orto položaju sa Rb;
Ra je halo, C1-4alkil, ili C1-4alkoksi;
Rb je triazol ili pirimidin supstituiran ili nesupstituiran sa halo ili C1-4alkil;
R2 je 6-člani heteroarilni prsten koji sadrži dva atoma dušika supstituirana sa jednim ili više članova izabranih iz grupe koju čine: halo, C1-4alkil, CD3, D, C1-4alkoksi, ciklopropil, morfolin-2-il, CO2C1-4alkil, CO2H, CH2OH, C(O)N(C1-4alkil)2, CF3, CN, OH, NO2, N(C1-4alkil)2, fenil, furan-2-il, tiofen2-il, 1H-pirazol-4-il, i pirolidin-1-il; ili farmaceutski prihvatljiva sol spoja formule (I), i barem jednu farmaceutski prihvatljivu pomoćnu tvar za upotrebu u postupku liječenja subjekta koji pati od ili kod kojeg je dijagnosticirana bolest, poremećaj ili medicinsko stanje posredovano aktivnošću receptora oreksina.
8. Barem jedan kemijski entitet i barem jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema zahtjevu 7, gdje je spomenuta bolest, poremećaj ili medicinsko stanje poremećaj ciklusa budnosti i sna, insomnije, sindroma nemirnih nogu, "jet lag", smetnje pri spavanju i poremećaj spavanja sekundaran neurološkom poremećaju.
9. Barem jedan kemijski entitet i barem jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema zahtjevu 8, gdje je spomenuta bolest, poremećaj ili medicinsko stanje insomnija.
10. Barem jedan kemijski entitet i barem jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema zahtjevu 8, gdje je spomenuta bolest, poremećaj ili medicinsko stanje poremećaj spavanja sekundaran depresiji.
11. Barem jedan kemijski entitet i barem jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema zahtjevu 8, gdje je spomenuta bolest, poremećaj ili medicinsko stanje poremećaj spavanja sekundaran demenciji.
12. Barem jedan kemijski entitet i barem jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema zahtjevu 8, gdje je spomenuta bolest, poremećaj ili medicinsko stanje poremećaj spavanja sekundaran Alzheimerovoj bolesti.
13. Barem jedan kemijski entitet i barem jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema bilo kojem od zahtjeva 8-12, gdje je spomenuti kemijski entitet [5-(4,6-dimetil-pirimidin-2-il)-heksahidro-pirol[3,4-c]pirol2-il]-(2-fluoro-6-[1,2,3]-triazol-2-il-fenil)metanon ili njegova farmaceutski prihvatljiva sol.
14. Barem jedan kemijski entitet i barem jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema bilo kojem od zahtjeva 8-12, gdje je spomenuti kemijski entitet HCI sol [5-(4,6-dimetil-pirimidin-2-il)-heksahidropirol[3,4-c]pirol-2-il]-(2-fluoro-6-[1,2,3]-triazol-2-il-fenil)metanona.
15. Barem jedan kemijski entitet i barem jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema bilo kojem od zahtjeva 8-12, gdje je spomenuti kemijski entitet [5-(4,6-dimetil-pirimidin-2-il)-heksahidro-pirol[3,4-c]pirol2-il]-(2-fluoro-6-[1,2,3]-triazol-2-il-fenil)metanon.
16. Barem jedan kemijski entitet i jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema bilo kojem od zahtjeva 8-12, gdje je spomenuti kemijski entitet 2-(4,6-dimetilpirimidin-2-il)-5-{[4-metoksi-2-(2H-1,2,3triazol-2-il)fenil]karbonil}oktahidropirolo[3,4-c]pirol ili njegova farmaceutski prihvatljiva sol.
17. Barem jedan kemijski entitet i jedna farmaceutski prihvatljiva pomoćna tvar za upotrebu prema bilo kojem od zahtjeva 8-12, gdje je spomenuti kemijski entitet 2-(4,6-dimetilpirimidin-2-il)-5-{[4-metoksi-2-(2H-1,2,3triazol-2-il)fenil]karbonil}oktahidropirolo[3,4-c]pirol.
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